It has been recently discovered that the natural product gambogic acid that is extracted from the gambogic resin of the Garcinia plant, is an effective ingredient in terms of anti-tumor characteristics. Research has shown that gambogic acid could selectively kill the various tumor cells without influencing the human hematopoietic or immune system. The gambogic acid could also combine with various proteins which are related to tumor formation and invasion, and thus induce apoptosis of the tumor cells. Therefore the gambogic acid could be used as an effective apoptosis inducer for various tumor systems. The formula of gambogic acid is shown below:

Due to the fact that the molecular weight of gambogic acid is relatively high, the presence of a corresponding group in modified structure might lead to undesired druggability, furthermore, the gambogic acid is obtained from natural products via extraction and separation, which does not facilitate industrial production. A structurally simplified analogue of the gambogic acid has been reported (Compound (II)), however, the anti-pharmaceutical test of the structurally simplified analogue of the gambogic acid (Compound (II)) showed that its anti-tumor activity is significantly reduced compared to the gambogic acid, thereby leading to poor medicinal properties. (Bioorganic & Medicinal Chemistry 16 (2008) pgs. 4233-4241).